B. Higgins

发表

Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy.

O. Myklebost, L. Vassilev, B. Vu, 2006, Proceedings of the National Academy of Sciences of the United States of America.

In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials

Qing Xiang, D. Heimbrook, C. Tovar, 2006, Molecular Cancer Therapeutics.

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

Kam Y. J. Zhang, K. Flaherty, J. Sosman, 2010, Nature.

Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.

Jing Zhang, Zhuming Zhang, Frank Podlaski, 2013, Journal of medicinal chemistry.

RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models.

D. Heimbrook, J. Grippo, B. Higgins, 2010, Cancer research.

High tumor levels of IL6 and IL8 abrogate preclinical efficacy of the γ‐secretase inhibitor, RO4929097

D. Carvajal, D. Heimbrook, B. Higgins, 2011, Molecular oncology.

Preclinical evaluation of tumor microvascular response to a novel antiangiogenic/antitumor agent RO0281501 by dynamic contrast-enhanced MRI at 1.5 T

Jonathan P. Dyke, Jason A. Koutcher, Brian Higgins, 2006, Molecular Cancer Therapeutics.

Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.

C. Lukacs, P. Rossman, P. Wovkulich, 2010, Bioorganic & medicinal chemistry letters.

Response of prostate cancer to anti-Her-2/neu antibody in androgen-dependent and -independent human xenograft models.

C. Cordon-Cardo, H. Scher, D. Agus, 1999, Cancer research.

In vivo activity of novel capecitabine regimens alone and with bevacizumab and oxaliplatin in colorectal cancer xenograft models

D. Heimbrook, B. Higgins, K. Kolinsky, 2009, Molecular Cancer Therapeutics.

Novel regimens of capecitabine alone and combined with irinotecan and bevacizumab in colorectal cancer xenografts.

D. Heimbrook, B. Higgins, K. Kolinsky, 2009, Anticancer research.

Advances in Brief 17-Allylamino-17-demethoxygeldanamycin Induces the Degradation of Androgen Receptor and HER-2 / neu and Inhibits the Growth of Prostate Cancer Xenografts 1

C. Cordon-Cardo, H. Scher, N. Rosen, 2002 .

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.

Yi Chen, K. Luk, A. Railkar, 2006, Bioorganic & medicinal chemistry letters.

Antitumor activity of capecitabine and bevacizumab combination in a human estrogen receptor-negative breast adenocarcinoma xenograft model.

D. Heimbrook, B. Higgins, K. Kolinsky, 2007, Anticancer research.

BRD4-mediated repression of p53 is a target for combination therapy in AML

M. Copland, K. Kirschner, T. Holyoake, 2020, bioRxiv.

Efficacy of vemurafenib (V), a selective V600EBRAF inhibitor, as monotherapy or in combination with erlotinib (Erl) or erbitux (Erb) and irinotecan (Iri) doublets and triplets in a colorectal cancer (CRC) xenograft model.

Richard J Lee, B. Higgins, K. Kolinsky, 2012, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

Efficacy of vemurafenib (V), a selective V600Eb-raf inhibitor, as monotherapy or in combination with erlotinib (Erl) or erbitux (Erb) and irinotecan (Iri) doublets and triplets in a colorectal cancer (CRC) xenograft model.

D. Heimbrook, B. Higgins, K. Kolinsky, 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

A potential role for activated HER-2 in prostate cancer.

H. Scher, M. Sliwkowski, D. Agus, 2000, Seminars in oncology.

MDM2 antagonists boost antitumor effect of androgen withdrawal: implications for therapy of prostate cancer

L. Vassilev, D. Heimbrook, C. Tovar, 2011, Molecular Cancer.

17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.

C. Cordon-Cardo, H. Scher, N. Rosen, 2002, Clinical cancer research : an official journal of the American Association for Cancer Research.

MDM2 Antagonists Counteract Drug-Induced DNA Damage

G. Ayers, D. Flaherty, Douglas B. Johnson, 2017, EBioMedicine.

MDM2 inhibition: an important step forward in cancer therapy

M. Konopleva, M. Andreeff, G. Martinelli, 2020, Leukemia.

Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.

L. Vassilev, B. Graves, Z. Filipovic, 2014, Bioorganic & medicinal chemistry.

RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.

K. Luk, A. Railkar, B. Higgins, 2005, Bioorganic & Medicinal Chemistry.

Cytoplasmic p53 couples oncogene-driven glucose metabolism to apoptosis and is a therapeutic target in glioblastoma

A. Letai, T. Cloughesy, P. Mischel, 2017, Nature Medicine.

Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer.

S. Kopetz, Richard J Lee, D. Heimbrook, 2012, Cancer research.

Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth.

Brian Higgins, H. Scher, M. Sliwkowski, 2002, Cancer cell.

Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.

Nader Fotouhi, Sung-Sau So, S. So, 2006, Journal of medicinal chemistry.

Phase I study of daily and weekly regimens of the orally administered MDM2 antagonist idasanutlin in patients with advanced tumors

J. Blay, Y. Bang, H. Hirte, 2021, Investigational New Drugs.

Murine double minute 2 inhibition alone or with cytarabine in acute myeloid leukemia: Results from an idasanutlin phase 1/1b study⋆.

W. Pierceall, G. Martinelli, B. Higgins, 2020, Leukemia research.

Functional dissection of transcriptional profiles in androgen-dependent and -independent prostate cancer

L. Sapinoso, S. Kern, G. Hampton, 2001, Nature Genetics.

Resistance to selective BRAF inhibition can be mediated by modest upstream pathway activation.

Qiongqing Wang, K. Trunzer, Richard J Lee, 2012, Cancer research.

BRAFV600E Negatively Regulates the AKT Pathway in Melanoma Cell Lines

B. Higgins, K. Packman, H. Niu, 2012, PloS one.

MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models.

Binh Vu, Frank Podlaski, Brian Higgins, 2013, Cancer research.

Antibody to vascular endothelial growth factor slows growth of an androgen-independent xenograft model of prostate cancer.

C. Cordon-Cardo, H. Scher, M. Drobnjak, 2002, Clinical cancer research : an official journal of the American Association for Cancer Research.

Phase 1/1b Study of RG7388, a Potent MDM2 Antagonist, in Acute Myelogenous Leukemia (AML) Patients (Pts)

W. Pierceall, G. Martinelli, B. Higgins, 2014 .

Phase 1 dose escalation, food effect, and biomarker study of RG7388, a more potent second-generation MDM2 antagonist, in patients (pts) with solid tumors.

J. Blay, Y. Bang, H. Hirte, 2014 .

Therapeutics , Targets , and Chemical Biology Identification of the MEK 1 ( F 129 L ) Activating Mutation as a Potential Mechanism of Acquired Resistance to MEK Inhibition in Human Cancers Carrying the B-Raf V 600 E Mutation

N. Rosen, D. Heimbrook, B. Higgins, 2011 .

Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy.

F. Podlaski, Norman Kong, N. Fotouhi, 2009, Cancer research.

Preclinical In vivo Evaluation of Efficacy, Pharmacokinetics, and Pharmacodynamics of a Novel MEK1/2 Kinase Inhibitor RO5068760 in Multiple Tumor Models

N. Fotouhi, A. Railkar, D. Heimbrook, 2010, Molecular Cancer Therapeutics.

Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models

B. Higgins, K. Kolinsky, E. Wheeldon, 2004, Anti-cancer drugs.

Preclinical Optimization of MDM2 Antagonist Scheduling for Cancer Treatment by Using a Model-Based Approach

L. Vassilev, Z. Filipovic, Kelli J. Glenn, 2014, Clinical Cancer Research.

Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.

S. So, L. Vassilev, B. Graves, 2014, ACS medicinal chemistry letters.

Phase Ib study of RG7112 with doxorubicin (D) in advanced soft tissue sarcoma (ASTS).

J. Blay, A. Cesne, A. Italiano, 2013 .

Suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses the growth of prostate cancer cells in vitro and in vivo.

R A Rifkind, C. Cordon-Cardo, H. Scher, 2000, Cancer research.

Inhibition of transformed cell growth and induction of cellular differentiation by pyroxamide, an inhibitor of histone deacetylase.

C. Cordon-Cardo, H. Scher, P. Marks, 2001, Clinical cancer research : an official journal of the American Association for Cancer Research.

Identification of the MEK1(F129L) activating mutation as a potential mechanism of acquired resistance to MEK inhibition in human cancers carrying the B-RafV600E mutation.

N. Rosen, D. Heimbrook, B. Higgins, 2011, Cancer research.

Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy

L. Vassilev, D. Heimbrook, C. Tovar, 2010, Cell cycle.

Phase 1 study of the MDM2 antagonist RO6839921 in patients with acute myeloid leukemia

B. Higgins, K. Yee, G. Uy, 2020, Investigational New Drugs.

A phase 1 study of the MDM2 antagonist RO6839921, a pegylated prodrug of idasanutlin, in patients with advanced solid tumors

W. Miller, B. Higgins, G. Uy, 2019, Investigational New Drugs.

Models Androgen-dependent and-independent Human Xenograft Response of Prostate Cancer to Anti-Her-2 / neu Antibody in Updated

C. Cordon-Cardo, H. Scher, D. Agus, 1999 .

Advances in Brief Response of Prostate Cancer to Anti-Her-2 / neu Antibody in Androgen-dependent and-independent Human Xenograft Models 1

C. Cordon-Cardo, H. Scher, D. Agus, 1999 .

Optimizing chemotherapy dose and schedule by Norton-Simon mathematical modeling.

Brian Higgins, Larry Norton, C. Hudis, 2010, Breast disease.

Preclinical testing of a novel regimen of capecitabine (C) in combination with bevacizumab (B) and trastuzumab (T) in a breast cancer xenograft model

C. Hudis, L. Norton, M. Theodoulou, 2007 .

Antitumor activity of HER1/EGFR tyrosine kinase inhibitor erlotinib, alone and in combination with CPT-11 (irinotecan) in human colorectal cancer xenograft models

Jianping Chen, B. Higgins, K. Kolinsky, 2007, Cancer Chemotherapy and Pharmacology.

Cancer Xenograft Model CWR 22-R Nonresponsive Genes in the Androgen-independent Prostate Dysregulated Expression of Androgen-responsive and Updated Version

S. Kern, G. Hampton, W. Gerald, 2000 .

Cancer Therapy : Preclinical Preclinical Optimization of MDM 2 Antagonist Scheduling for Cancer Treatment by Using a Model-Based Approach

L. Vassilev, Z. Filipovic, Kelli J. Glenn, 2014 .

Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.

K. Luk, P. Wovkulich, C. Tovar, 2013, ACS medicinal chemistry letters.

Preclinical evaluation of the novel multi-targeted agent R1530

D. Carvajal, A. Railkar, P. Wovkulich, 2011, Cancer Chemotherapy and Pharmacology.